Thiazolidinediones of omega-3 polyunsaturated acids as new insulin sensitizers for treating type2 diabetes

摘要

The present invention relates to thiazolidinedione derivatives of omega-3 fatty acids as insulin sensitizers, and their use in treating Type2 diabetes, obesity, hypertriglyceridemia, cardiovascular diseases, metabolic diseases, inflammation, renal anemia, and/or Alzheimer's disease: and for modulating activity of peroxisome proliferator-activated receptors (PPARs).

主权项

1. Compounds of Formula (I) wherein: R is joined from the methylene moiety formed by reduction of the carboxylic acid of one of the following acids: cis,cis,cis-7,10,13-hexadecatrienoic acid (HTA), named as RS-5-((7Z,10Z,13Z)-hexadeca-7,10,13-trien-1-yl)thiazolidine-2,4-dione; cis,cis,cis-9,12,15-octadecatrienoic acid (ALA), named as RS-5-(9Z,12Z,15Z)-octadeca-6,9,12-trien-1-yl)thiazolidine-2,4-dione; cis,cis,cis,cis-6,9,12,15-octadecatetraenoic acid (SDA), named as RS-5-((6Z,9Z,12Z,15)-octadeca-6,9,12,15-tetraen-1-yl)thiazolidine-2,4-dione; cis,cis,cis-11,14,17-eicosatrienoic acid (ETE), named as RS-5-((11Z,14Z,17Z)-eicosa-11,14,17-triene-1-yl)thiazolidine-2,4-dione; cis,cis,cis,cis-8,11,14,17-eicosatetraenoic acid (ETA), named as RS-5-((8Z,11Z,14Z,17Z)-eicosa-8,11,14,17-tetraen-1-vi)thiazoliidine-2,4-dione; cis,cis,cis,cis,cis-5,8,11,14,17-eicosapentanenoic acid (EPA), named as RS-5-((5Z,8Z,11Z,14Z,17Z)-eicosa-5,8,11,14,17-pentaen-1-yl)thiazolidine-2,4-dione; cis,cis,cis,cis,cis-6,9,12,15,18-heneicosapentaenoic acid (HPA), named as RS-5-((6Z,9Z,12Z,15Z,18Z)-heneicosa-6,9,12,15,18-pentaen-1-yl)thiazolidine-2,4-dione: cis,cis,cis,cis,cis-7,10,13,16,19-docosapentaenoic acid (DPA), named as RS-5-((7Z,10Z,13Z,16Z,19Z)docosa-7,10,13,16,19-pentaen-1-yl)thiazolidine-2,4-dione; cis,cis,cis,cis,cis,cis-4,7,10,13,16,19-docosahexaenoic acid (DHA), named as RS-5-((4Z,7Z,10Z,13Z,16Z,19Z)docosa-4,7,10,13,16,19-hexaen-1-yl)thiazolidine-2,4-dione; cis,cis,cis,cis,cis-9,12,15,18,21-tetracosapentaeonic acid (TPA), named as RS-5-((9Z,12Z,15Z,18Z,21Z)-tetracosa-9,12,15,18,21-pentaen-1-yl)thiazolidine-2,4-dione; or cis,cis,cis,cis,cis,cis-6,9,12,15,18,21-tetracosahexaeonic acid (THA), named as RS-5-((6Z,9Z,12Z,15Z,18Z,21Z)-tetracosa-6,9,12,15,18,21-hexaen-1-yl)thiazolidine-2,4-dione.